(19)
(11) EP 0 137 746 A3

(12) EUROPEAN PATENT APPLICATION

(88) Date of publication A3:
08.01.1986 Bulletin 1986/02

(43) Date of publication A2:
17.04.1985 Bulletin 1985/16

(21) Application number: 84306256

(22) Date of filing: 13.09.1984
(84) Designated Contracting States:
AT BE CH DE FR GB IT LI LU NL SE

(30) Priority: 22.09.1983 GB 8325465
26.11.1983 GB 8331643
07.02.1984 GB 843217
07.02.1984 GB 843218
12.05.1984 GB 8412183

(71) Applicant: FISONS plc
 ()

(72) Inventor:
  • Robinson, David Hulme
     ()

   


(54) Nitrogen substituted angiotensin converting enzyme inhibitors


(57) There are described compounds of formula I,

in which

Z is R2CH (COOH) NH- or R1SCH2-,

R1is hydrogen or R8CO-,

R8 is alkyl C1 to 10 or phenyl,

R is hydrogen, alkyl C1 to 6, or alkyl C1 to 6 substituted by phenyl, -NH2, -COOH or by alkyl C1 to 6 thio,

R2 is hydrogen, alkyl C1 to 10, cycloalkyl C3 to 10, phenyl, phenylalkyl C7 to 12, alkoxy C1 to 6 - alkyl C1 to 6, alkyl C1 to 6 - thioalkyl C1 to 6, phenyloxyalkyl C7 to 12 or phenylthioalkyl C7 to 12,

R. and R5, which may be the same or different, are each hydrogen, alkyl C1 to 10, cycloalkyl C3 to 10, phenylalkyl C7 to 12, or phenyl; the phenyl and phenylalkyl each optionally being substituted by one or more alkyl C1 to 6, alkoxy C1 to 6 or halogen groups, or

R. and R5 together form a - (CH2),,- or - (CW2)5- chain, and

R6 is hydrogen, alkyl C1 to 6 or phenylalkyl C7 to 12, and pharmaceutically acceptable salts and esters thereof.


There are also described processes for making the compounds and their formulation and use as pharmaceuticals, eg. angiotensin converting enzyme inhibitors.





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